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BQ-788 sodium salt

Cat. No. M13959
BQ-788 sodium salt Structure
Size Price Availability Quantity
5mg USD 400  USD400 In stock
10mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

BQ-788 sodium salt is an effective and selective ETB receptor antagonist with an IC50 of 1.2 nM in human Girrardi heart cells to inhibit ET-1 binding to the ETB receptor. BQ-788 is an enhancer of AQP4(Aquaporin-4).

Chemical Information
Molecular Weight 663.78
CAS Number 156161-89-6
Solubility (25°C) DMSO ≥ 43 mg/mL
Storage -20°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Aso Saeed, et al. Effects of endothelin receptor antagonists on renal hemodynamics in angiotensin II-infused rats on high NaCl intake

[2] Jean-Philippe Brosseau, et al. Development of an efficient strategy for the synthesis of the ETB receptor antagonist BQ-788 and some related analogues

[3] M Bays, et al. Gateways to Clinical Trials

[4] K Sato, et al. Mechanism of hypoxic pulmonary vasoconstriction involves ET(A) receptor-mediated inhibition of K(ATP) channel

[5] M Muramatsu, et al. Endothelin-1 mediates nitro-L-arginine vasoconstriction of hypertensive rat lungs

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Keywords: BQ-788 sodium salt supplier, Endothelin Receptor, inhibitors, activators


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